Brand Name :
ACT Cabergoline,Dostinex, APO Cabergoline
Synonyms :
cabergoline
Class :
Hyperprolactinemia, Dopamine agonist
Brand Name :
ACT Cabergoline,Dostinex, APO Cabergoline
Synonyms :
cabergoline
Class :
Hyperprolactinemia, Dopamine agonist
Dosage Forms & Strengths
tablet
0.5mg
Initial dose:0.25mg orally twice a week
Can increase by 0.25mg every four weeks up to 1mg twice a week
Safety and efficacy not established
Refer adult dosing
acrivastine and pseudoephedrine
may increase the vasoconstrictive effect of alpha/beta agonists
may decrease the vasodilatory effect when combined with nitroglycerin
they increase the effect of vasoconstriction of alpha-1 agonists
may increase the vasoconstriction effect
may increase the vasoconstriction effect
may increase the vasoconstriction effect
may increase the vasoconstriction effect
may increase the vasoconstriction effect
may decrease the therapeutic effect of cabergoline
may decrease the therapeutic effect of cabergoline
may decrease the therapeutic effect of cabergoline
may decrease the therapeutic effect of cabergoline
may decrease the therapeutic effect of cabergoline
may increase the toxic effect of ergot derivatives
may increase the toxic effect of ergot derivatives
may increase the toxic effect of ergot derivatives
may increase the vasoconstricting effect of ergot derivatives
may decrease the therapeutic effect of cabergoline
it decreases the effects of antipsychotic agents
it decreases the effects of antipsychotic agents
it decreases the effects of antipsychotic agents
it decreases the effects of antipsychotic agents
it decreases the effects of antipsychotic agents
may have an increased vasoconstricting effect when combined with alpha1-agonists
it decreases the effect of antipsychotic agents
it decreases the effect of metoclopramide
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may enhance the vasoconstricting effect of ergot Derivatives
may increase the vasoconstriction effect of sympathomimetic drugs
may increase the vasoconstriction effect of sympathomimetic drugs
may enhance the serum concentration of CYP3A4 inhibitors
may diminish the therapeutic effect of antipsychotic agents
may enhance the serum concentration of CYP3A4 inhibitors
may increase the levels of serum concentration of ergot derivatives
may increase the levels of serum concentration of ergot derivatives
may increase the levels of serum concentration of ergot derivatives
may increase the levels of serum concentration of ergot derivatives
may increase the levels of serum concentration of ergot derivatives
may increase the levels of serum concentration of ergot derivatives
may increase the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists (Triptans)
ergot Derivatives may enhance the serotonergic effect of serotonergic Agents
Beta-Blockers increase the effect of vasoconstriction of ergot derivatives
Beta-Blockers increase the effect of vasoconstriction of ergot derivatives
Beta-Blockers increase the effect of vasoconstriction of ergot derivatives
Beta-Blockers increase the effect of vasoconstriction of ergot derivatives
Beta-Blockers increase the effect of vasoconstriction of ergot derivatives
may increase the serum concentration of cabergoline
may increase the serotonergic effect of ergot derivatives
may increase the vasoconstricting effect of ergot derivatives
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
it may increase the effect of serotonergic agents
beta-blockers may enhance the vasoconstricting effect of ergot derivatives
beta-blockers may enhance the vasoconstricting effect of ergot derivatives
beta-blockers may enhance the vasoconstricting effect of ergot derivatives
beta-blockers may enhance the vasoconstricting effect of ergot derivatives
beta-blockers may enhance the vasoconstricting effect of ergot derivatives
may increase the serum concentration of ergot derivatives
may increase the serum concentration of ergot derivatives
may increase the serum concentration of ergot derivatives
may increase the serum concentration of ergot derivatives
may increase the serum concentration of ergot derivatives
may increase the vasoconstrictive effect of beta blockers
may increase the effect of ergot derivatives
may increase the effect of ergot derivatives
may increase the effect of ergot derivatives
may increase the effect of ergot derivatives
may increase the effect of ergot derivatives
may increase the vasoconstricting effect
may increase the vasoconstricting effect
may increase the vasoconstricting effect
may increase the vasoconstricting effect
may increase the vasoconstricting effect
may increase the serum concentration
may increase the vasoconstricting effect
Mechanism of action
The action of cabergoline stimulates the dopamine receptors in the pituitary gland, reducing the secretion of prolactin from the lactotroph cells. This reduction in prolactin secretion is responsible for the drug’s therapeutic effects in hyperprolactinemia and other conditions associated with elevated prolactin levels
In Parkinson’s disease, cabergoline works by enhancing the effect of dopamine in the brain and improving the symptoms of the disease, such as tremors, rigidity, and bradykinesia
Spectrum
It has a broad spectrum of activity, which is why it treats various conditions. In addition to hyperprolactinemia and Parkinson’s disease, cabergoline has also been used to treat infertility, uterine fibroids, and obsessive-compulsive disorder
Frequency defined:
>10%
headache (26%)
nausea (27%)
dizziness (15%)
1-10%
fatigue (7%)
somnolence (5%)
depression (3%)
nervousness (2%)
breast pain (1%)
hot flashes (1%)
constipation (10%)
asthenia (9%)
abdominal pain (5%)
postural hypotension (4%)
dyspepsia (2%)
abnormal vision (1%)
dysmenorrhea (1%)
paresthesia (1%)
<1%
fibrosis
valvulopathy
pleural effusion
aggression
gastric ulcer
psychosis
Post-marketing reports
increased libido and pathological gambling
hypersexuality
Contraindications
Caution
There are several cautions and potential side effects associated with its use:
Pregnancy consideration: B
Lactation: Excretion of the drug in human breast milk is unknown
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology
cabergoline has a long half-life and is taken orally, usually once or twice a week. After oral administration, it is absorbed rapidly and reaches peak plasma concentrations in about 2-5 hours. cabergoline is highly lipophilic and is widely distributed throughout the body, including the central nervous system. It is primarily metabolized in the liver and excreted in the urine
The main therapeutic effect of cabergoline is its ability to lower elevated prolactin levels in patients with hyperprolactinemia. By decreasing prolactin secretion, cabergoline can alleviate symptoms such as infertility, galactorrhea, and hypogonadism. cabergoline is also used to treat Parkinson’s disease by increasing dopamine levels in the brain, which can improve motor symptoms such as tremors and rigidity
Pharmacodynamics
The pharmacodynamics of cabergoline can be described as follows:
Pharmacokinetics
Absorption
cabergoline is rapidly absorbed after oral administration and reaches peak plasma concentrations in about 2-3 hours. The half-life of cabergoline is approximately 63-69 hours, which allows for once or twice weekly dosing. The peak plasma concentration of cabergoline is typically 30-70 pg/mL following single oral doses of 0.5-1.5 mg
Distribution
cabergoline is highly lipophilic and is widely distributed throughout the body, including the central nervous system. It is bound to 40-42% of plasma proteins
Metabolism
It is extensively hydrolyzed in the liver by a variety of enzymes. The primary metabolites of cabergoline are inactive and do not contribute to its therapeutic effects
Elimination/Excretion
It is excreted primarily in the feces (60%) and, to a lesser extent, in the urine (22%). The half-life of cabergoline is approximately 63-69 hours, which allows for once or twice weekly dosing
Administration
Hyperprolactinemia: For the treatment of hyperprolactinemia, the usual starting dose of cabergoline is 0.5 mg once or twice a week. The dose may be increased as needed, up to 2 mg per week
Parkinson’s disease: For treating Parkinson’s disease, the starting dose of cabergoline is 0.5 mg twice a week. The dose may be increased as needed, up to 5 mg per week
Dosing frequency: cabergoline has a long half-life, which allows for once or twice weekly dosing. The frequency of administration may be adjusted based on the response of the patient and the severity of the condition being treated
Timing of administration: cabergoline should be taken simultaneously daily, with or without food. It is essential to follow the doctor’s dosing schedule and not take more or less of the medication than prescribed
Missed doses: If a dose is missed, it should be taken as soon as possible. If it is almost time for the next dose, the missed dose should be skipped, and the next dose should be taken regularly
Patient information leaflet
Generic Name: cabergoline
Pronounced: [ ca-BER-goe-leen ]
Why do we use cabergoline?